Correas J M, Meuter A R, Singlas E, Kessler D R, Worah D, Quay S C
Department of Radiology, University Hospital of Necker, Paris, France.
Ultrasound Med Biol. 2001 Apr;27(4):565-70. doi: 10.1016/s0301-5629(00)00363-x.
The purpose of this study was to prospectively study the human pharmacokinetics of an ultrasound (US) contrast agent through its active ingredient, dodecafluoropentane (DDFP). Expired air and blood samples were collected from 24 volunteers after IV administration from 0.01 to 0.1 mL/kg. They were analyzed by a gas chromatographic method specially adapted to the study of DDFP. Blood data fitted to an open one-compartment model. Elimination half-life range was 1.8 to 2.5 min. The area under the curve was correlated to the dose (r(2) = 0.99). Mean blood clearance ranged from 30 to 49 mL/min kg. Blood apparent distribution volume ranged from 0.09 to 0.15 L/kg. In expired air, DDFP concentration exhibited a biexponential decay. The percentage of recovery was 98 +/- 19% at 2 h. No extraneous peaks were observed, indicating no detectable DDFP metabolites. It was concluded that DDFP pharmacokinetics in blood fitted to an open one-compartment model with a fast elimination half-life. Recovery in expired air was almost complete 2 h after administration.
本研究的目的是通过其活性成分十二氟戊烷(DDFP)对超声(US)造影剂的人体药代动力学进行前瞻性研究。从24名志愿者静脉注射0.01至0.1 mL/kg后采集呼出气和血样。采用专门适用于DDFP研究的气相色谱法对其进行分析。血液数据符合开放一室模型。消除半衰期范围为1.8至2.5分钟。曲线下面积与剂量相关(r(2) = 0.99)。平均血液清除率范围为30至49 mL/min·kg。血液表观分布容积范围为0.09至0.15 L/kg。在呼出气中,DDFP浓度呈现双指数衰减。给药2小时后回收率为98±19%。未观察到额外峰,表明未检测到DDFP代谢物。结论是血液中DDFP的药代动力学符合具有快速消除半衰期的开放一室模型。给药2小时后呼出气中的回收几乎完全。